atp citrate lyase

Hydroxycitric acid tripotassium hydrate (Potassium citrate monohydrate) 是一种藤黄果的主要活性成分，也是一种柠檬酸的衍生物。它可竞争性抑制柠檬酸裂解酶 (ATP citrate lyase) ，并具有减肥作用。它有效抑制结石形成，并抑制HIF，具有抗氧化，抗炎和抗肿瘤活性。

2-Furoic acid (Furan-2-carboxylic acid) 2-Furoic acid 能够降低血清中胆固醇和甘油三酯的水平，具有抗血脂作用。

(-)-Hydroxycitric acid (Garcinia acid) 是Garcinia cambogia 果皮中的主要酸。它是 ATP 柠檬酸裂解酶的竞争性抑制剂，能够抑制脂肪酸的合成，减少脂肪生成，控制食物摄入，从而减轻体重。

Forrestiacids K, 萜类化合物，源自Pseudotsuga forrestii，作为ATP-citrate lyase (ACL) 的抑制剂。

Forrestiacids J为一种特异性抑制ATP-柠檬酸裂解酶 (ACL) 的化合物，其IC50值为2.6 μM。

BMS-303141是高效性和可渗透细胞的 ACL 抑制剂(IC50:0.13 μM)。

SB 204990是一种有效的、特异性 ATP 柠檬酸裂解酶抑制剂 SB-201076 的内酯前药。

(-)-Hydroxycitric acid lactone (Garcinia lactone) 是一种有效的 ATP-柠檬酸裂解酶抑制剂，能够催化柠檬酸盐线粒体外裂解为草酰乙酸和乙酰辅酶 A，限制了脂肪酸合成所需乙酰辅酶 A 单位的可用性。它是一种减肥药，是一种广受欢迎的减肥食品补充剂。

Bempedoic acid (ETC1002) 是一种 ATP-柠檬酸裂解酶抑制剂，可激活AMPK。它是脂质和碳水化合物代谢的调节剂。

NDI-091143 是高亲和力人 ATP 柠檬酸裂解酶抑制剂，其IC50为 2.1 nM (ADP-Glo 分析)，Ki 为 7.0 nM，Kd 为 2.2 nM。它能够稳定柠檬酸盐域中的大构象变化，间接抑制柠檬酸的结合和识别，进而抑制ACLY 催化变构反应。

Citric acid trilithium salt tetrahydrate (Lithium citrate tribasic tetrahydrate) 是一种用于治疗精神疾病的药物。它也是一种医药和建筑材料, 可用于氨基酸定量分析时的梯度洗脱。

MEDICA16 是 GPR40 的特异性激动剂以及 GPR120 的部分激动剂。 MEDICA16 是一种 ATP-柠檬酸裂解酶抑制剂，可显着降低腓肠肌中的细胞内 TG 含量，同时增加胰岛素敏感性。

ACLY inhibitor 7（compound 7）对human ATP citrate lyase（hACLY）具有抑制作用，使用 ADP-Glo测试得出的IC50< 1 nM。

Antimycin A4 is an active component of the antimycin A antibiotic complex that is more polar than antimycin A1 , antimycin A2 , and antimycin A3 . Antimycin A4 inhibits ATP-citrate lyase with a Ki value of 64.8 μM. The antimycin A complex is a mixture of antimycins A1, A2, A3, and A4 that demonstrates antifungal, insecticidal, nematocidal, and piscicidal properties. It blocks mitochondrial respiration and can deplete cellular levels of ATP via inhibition of complex III of the mitochondrial electron transport chain (ETC). Antimycin A prevents the transfer of electrons between the b-cytochromes and ubiquinone at the Q(inner) site of complex III. This results in the stabilization of the ubisemiquinone radical at the Q(outer) site of complex III, leading to increased production of superoxide. Antimycin A is widely used in research to shunt electron flow through the ETC to study the chemical details of oxygen respiration. Additionally, antimycin A has been shown to inhibit Bcl-2 and Bcl-xL proteins, inducing apoptosis.

SB-201076 is a potent ATP citrate-lyase inhibitor. SB-204990 is the prodrug of SB-201076.

Nicodicosapent is a fatty acid niacin conjugate. It is also an inhibitor of the sterol regulatory element-binding protein (SREBP). The sterol regulatory element-binding protein (SREBP) is a key regulator of cholesterol metabolism proteins such as PCSK9, H

(-)-Hydroxycitric acid (HCA) can inhibit fat synthesis and reduces food intake, the primary mechanism of action of HCA appears to be related to its ability to act as a competitive inhibitor of the enzyme ATP-citrate lyase, which catalyzes the conversion of citrate and coenzyme A to oxaloacetate and acetyl coenzyme A (acetyl-CoA), primary building blocks of fatty acid and cholesterol synthesis.

Palmitoleic acid, an ω-7 monounsaturated fatty acid found in macadamia and sea buckthorn oils, enhances both basal and insulin-stimulated glucose uptake, as well as Glut4 protein levels in 3T3-L1 adipocytes at a 200 µM concentration. Ex vivo, at a dosage of 300 mg kg per day, it significantly increases glucose uptake and both aerobic and anaerobic glycolysis, while decreasing de novo fatty acid synthesis and the activity of lipogenic enzymes, specifically ATP citrate lyase (ACL) and glucose-6-phosphate dehydrogenase (G6PDH), in isolated murine adipocytes. Furthermore, the dietary administration of palmitoleic acid at 300 mg kg mitigates high-fat diet-induced insulin resistance and liver inflammation in mice.

Gnetuhainin I (Compound 5)是源自Pouzolzia zeylanica的木质素化合物，展现出对ATP柠檬酸裂解酶（ACLY）的显著抑制效果，其半抑制浓度（IC50）值为2.63 μM。